ActiTarg Series · 6,600+ compounds
ActiTarg-K Kinase Modulators
Kinase modulators from TimTec stock (6,600+ compounds), including the 960-compound K960 diversity subset for smaller screens.
ActiTarg-K is a screening set of kinase modulators from TimTec stock lattices associated with published kinase activity. The full collection contains 6,600+ compounds across a variety of chemical series. Structural constraints and novel pendants provide variability for hit optimization. A 960-compound diversity subset, ActiTarg-K960, is a pre-filtered 12-plate set for smaller kinase screens. Compounds are available for cherry-picking and/or as a collection in 96- or 384-well plates and in vials.
Among strategies in cancer therapeutics, protein kinase inhibition is a viable approach, stimulated by the role this family of phosphorylating enzymes plays in proliferative processes and by agents such as imatinib (Gleevec) in chronic myeloid leukemia and certain solid tumors. Along with that tyrosine kinase inhibitor, other agents that inhibit this and other cell-cycle-regulating kinases (CDKs) have been developed for cancer and immune-system disorders.
Lattices represented
| Kinase context | Lattice type |
|---|---|
| Tyrosine / CDK | Various |
| CDK | Adenines; flavones; isoflavones; 2-aminothiazoles |
| p38 MAP | 4,5-Diarylimidazoles |
| Raf | Diarylureas |
| Ser/Thr | NaphthSONH |
| PASS* >0.50 subsets | CDK isoxazolidinine and aminothiazole; tyrosine; p38MAP; PKC |
*PASS: software that predicts biological activity based on structural similarity to compounds reported to have the specified activity.
Published screens that used ActiTarg-K
These are literature reports, not TimTec efficacy claims:
- Zeng, G.; Bueno, M.; Camachos, C. J.; Ramaswami, B.; Luo, C.; Randhawa, P. Validation of BKV large T-antigen ATP-binding site as a target for drug discovery. Antiviral Res. 2009, 81(2), 184–187. doi:10.1016/j.antiviral.2008.11.004. Pilot screen of 300 compounds from the TimTec ActiTarg-K library (written “Tim Tec ActiTarg K”).
- Vornhagen, J.; Burnside, K.; Whidbey, C.; Berry, J.; Qin, X.; Rajagopal, L. Kinase inhibitors that increase the sensitivity of methicillin resistant Staphylococcus aureus to β-lactam antibiotics. Pathogens 2015, 4(4), 708–721. doi:10.3390/pathogens4040708. 280-compound TimTec kinase-inhibitor set; methods cite the ActiTarg-K product URL.
- Lagerweij, T.; Hiddingh, L.; et al. A chemical screen for medulloblastoma identifies quercetin as a putative radiosensitizer. Oncotarget 2016, 7(24), 35776–35788. doi:10.18632/oncotarget.7980. ActiTarg-K960 (960 putative kinase inhibitors) obtained from TimTec.
- Druzhyna, N.; et al. Screening of a composite library of clinically used drugs and well-characterized pharmacological compounds for cystathionine β-synthase inhibition identifies benserazide as a drug potentially suitable for repurposing for the experimental therapy of colon cancer. Pharmacol. Res. 2016, 113, 18–37. doi:10.1016/j.phrs.2016.08.016. Composite screen included ActiTarg-K (960 kinase modulators) from TimTec.
- Kolluru, S.; Momoh, R.; Lin, L.; Mallareddy, J. R.; Krstenansky, J. L. Identification of potential binding pocket on viral oncoprotein HPV16 E6: a promising anti-cancer target for small molecule drug discovery. BMC Mol. Cell Biol. 2019, 20:30. doi:10.1186/s12860-019-0214-3. Screened the ActiTarg-K Library (TimTec).
- Serra-Roma, A.; Shakhova, O. Identification of novel small-molecule kinase modulators for the treatment of neuroblastoma. Oncol. Ther. 2020. doi:10.1007/s40487-020-00113-5. HTS of ActiTarg-K960 (TimTec Inc.), the 960-compound diversity subset of ActiTarg-K.
- Eichhoff, O. M.; et al. ROS induction targets persister cancer cells with low metabolic activity in NRAS-mutated melanoma. Cancer Res. 2023, 83(7), 1128–1146. doi:10.1158/0008-5472.CAN-22-1826. ActiTarg-K kinase modulators (TimTec); the associated preprint names the ActiTarg-K Kinase Modulators Library.
ActiTarg is one of TimTec’s targeted series. See the ActiTarg Series for the other letter collections.